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Caroline M Gorvin

type 5, which is characterised by renal salt wasting, hypokalaemia, hyperreninaemia and hyperaldosteronaemia ( Vargas-Poussou et al . 2002 , Watanabe et al . 2002 ). Biased signalling of the CASR Functional studies in HEK293 cells have

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Hui Huang and Ya-Xiong Tao

). The existence of biased signaling has been reported in multiple GPCRs with important therapeutic implications (for reviews, see Violin & Lefkowitz (2007) , Rajagopal et al . (2010) and Reiter et al . (2012) ). In addition to biased ligands

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Xiu-Lei Mo, Rui Yang and Ya-Xiong Tao

signal through both cAMP and ERK1/2 and because the ERK1/2 signaling pathway has been suggested to be one cellular mechanism underlying the regulation of energy homeostasis by MC4R ( Sutton et al . 2005 ), we asked whether there is biased signaling at

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Zhao Yang, Zhi-Li Huang and Ya-Xiong Tao

. 2012 ) (one report suggested that the MC3R does not activate ERK1/2 ( Daniels et al . 2003 )). However, we and others recently reported biased signaling in the MC3R ( Huang & Tao 2014 , Montero-Melendez et al . 2015 , Yang et al . 2015 ), the ERK1

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Pál Gyombolai, András D Tóth, Dániel Tímár, Gábor Turu and László Hunyady

of the curves ( Fig. 4 G, H and Table 1 ). These results suggest that the signaling of this mutant is shifted from G-protein activation toward β-arr2 recruitment, and therefore CB 1 R-AAY can be considered as a β-arr2-biased mutant. The

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Hui Huang and Ya-Xiong Tao

(10 −5  M α- or β-MSH stimulation) and ERK1/2 phosphorylation (10 −6  M NDP-MSH stimulation). Basal signaling in both pathways was also decreased compared with the WT receptor. No apparent biased signaling (see below) was observed. The basal activities

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Caroline M Gorvin

ligand than WT receptor ( Fig. 6E ) ( Zhang et al. 2014 , Geng et al. 2016 , Zhang et al. 2016 ). Consistent with such mutations favouring a partially active state, rather than enhancing protein levels or biasing signalling, when expressed in

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Davide Calebiro, Viacheslav O Nikolaev and Martin J Lohse

done mostly in the 1980s using cells, cell membrane preparations, and reconstituted systems with purified proteins has revealed the basic structure and functional properties of GPCR signaling cascades. They consist of a receptor, a heterotrimeric G

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J Jason Collier, Tim E Sparer, Michael D Karlstad and Susan J Burke

receptor trigger differential downstream effects ( Zweemer et al . 2014 ). In other words, one receptor can produce distinct outcomes depending on which ligand occupies the binding site. This updated paradigm is often referred to as biased signaling

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Carolin L Piechowski, Anne Rediger, Christina Lagemann, Jessica Mühlhaus, Anne Müller, Juliane Pratzka, Patrick Tarnow, Annette Grüters, Heiko Krude, Gunnar Kleinau and Heike Biebermann

) basal tone of signaling (cAMP accumulation), such as mutations at Leu140 in TMH3 ( Mo et al . 2012 ). It has also been reported that specific mutations may induce biased signals, whereby cAMP accumulation related to Gs and to the pERK1/2 pathway can be